Abstract
A series of 81 3-phenyl-2H-benzoxazine-2,4(3H)-diones with substitution at C(6) on the benzoxazine ring and on the phenyl moiety was synthesized; the compounds were evaluated for antifungal activity against five strains of potentially pathogenic fungi (Absidia corymbifera, Aspergillus fumigatus, Candida albicans, Microsporum gypseum andTrichophyton mentagrophytes). Structure-activity relationships againstT. mentagrophytes andM. gypseum were determined using the Free-Wilson method, which was further combined with the approach of Hansch.In vitro antifungal activity becomes higher with increasing electron-accepting ability of the substituents on the phenyl ring, and with increasing lipophilicity.
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Dedicated to Prof. RNDr. Bolumil Sikyta, DrSc., on the occasion of his 70th birthday
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Waisser, K., Kubicová, L., Buchta, V. et al. In vitro antifungal activity of 3-phenyl-2H-benzoxazine-2,4(3H)-diones. Folia Microbiol 47, 488–492 (2002). https://doi.org/10.1007/BF02818786
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DOI: https://doi.org/10.1007/BF02818786